| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MIC50: 0.12 mg/L(P. aeruginosa)[2] MIC90: 0.12 mg/L(P. aeruginosa)[2] IC50: 5.84 μM (gentamicin)[2]
Murepavadin TFA targets the lipopolysaccharide (LPS) transport protein D (LptD) on the outer membrane of Pseudomonas aeruginosa. By binding to LptD, it disrupts LPS transport to the outer membrane, compromising bacterial cell envelope integrity and leading to bacterial death through a non-lytic, non-membrane-disruptive mechanism. |
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| ln Vitro |
Murepavadin is active against P. aeruginosa, as evidenced by its 0.12 mg/L MIC50 and MIC90 values[2]. With an IC50 value of 5.84 μM, murepavadin inhibits the absorption of gentamicin by megalin in vitro[2].
Murepavadin TFA demonstrates potent and specific antibacterial activity against Pseudomonas aeruginosa with MIC50 and MIC90 values both measured at 0.12 mg/L (approximately 0.07 microM). It exhibits activity against a broad panel of multi-drug-resistant P. aeruginosa isolates and is highly selective for this species, showing minimal activity against other Gram-negative or Gram-positive bacteria. |
| ln Vivo |
In preclinical animal models, including infection with XDR isolates, murepavadin (sc; 0-100 mg/kg) is effective [2].
In preclinical infection models using extensively drug-resistant (XDR) bacterial isolates, subcutaneous administration of Murepavadin TFA (0-100 mg/kg) demonstrated significant antibacterial activity. It effectively reduces bacterial load and improves survival in animal models of P. aeruginosa infection. It also activates mast cells via MRGPRX2 and MrgprB2, inducing Ca2+ mobilization and degranulation. |
| Enzyme Assay |
Not applicable. Murepavadin TFA targets a bacterial protein, not a mammalian receptor. Standard binding assays involve surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure binding affinity to purified LptD protein. Alternatively, bacterial membrane permeability assays using fluorescent probes (e.g., NPN uptake) assess outer membrane disruption.
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| Cell Assay |
A standard cellular protocol for antibacterial susceptibility testing follows CLSI guidelines: P. aeruginosa isolates are cultured in Mueller-Hinton broth, and a 2-fold dilution series of Murepavadin TFA (0.004-256 mg/L) is prepared in 96-well plates. Bacterial inoculum (5×10⁵ CFU/mL) is added, and plates are incubated at 35degC for 16-20 hours. The MIC is determined as the lowest concentration with no visible growth. MIC50 and MIC90 values are calculated from multiple isolates.
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| Animal Protocol |
Animal/Disease Models: Murine models of P. aeruginosa infection[2]
Doses: 0-100 mg/kg Route of Administration: Subcutaneous, q24h or q12h Experimental Results: Resulted in an increase in survival rate to 100% and demonstrated Dramatically lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection. Animal/Disease Models: Mouse, rat, rabbit, and monkey[2] Doses: 0-5 mg/kg Route of Administration: intraperitoneal (ip)or subcutaneous, single Experimental Results: Followed a two-compartment model following intravenous (iv) administration and decline of plasma concentrations. Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) . Had high bioavailability (67.79 %) after subcutaneous (sc) administration in rats but had low oral bioavailability (<0.01%). Had a linear relationship between ELF AUC and unbound plasma AUC in mouse. Did not readily cross the blood/brain barrier. A standard in vivo protocol involves establishing a neutropenic mouse model of P. aeruginosa infection by cyclophosphamide treatment (150 mg/kg on days -4 and -1), followed by intraperitoneal or intratracheal bacterial inoculation (1×10⁵-1×10⁶ CFU). Murepavadin TFA (0-100 mg/kg) is administered subcutaneously 1 hour post-infection, with additional doses every 6-12 hours. Efficacy endpoints include survival rate over 7 days, bacterial burden (CFU) in lungs and blood, and cytokine levels. |
| ADME/Pharmacokinetics |
As a 14-amino-acid cyclic peptide, Murepavadin TFA has a molecular weight of 1667.83. It is typically administered subcutaneously or intravenously. The peptide has a relatively short half-life (minutes to hours) due to proteolytic degradation. Its pharmacokinetics are characterized by dose-proportional exposure, and it is primarily eliminated via renal clearance.
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| Toxicity/Toxicokinetics |
The primary toxicities of Murepavadin in preclinical studies are related to its on-target antibacterial activity and potential immunomodulatory effects. It activates mast cells via MRGPRX2, which can lead to histamine release and allergic-type reactions. Clinical studies have reported nephrotoxicity at higher doses. Murepavacin toxicity is typically manageable at therapeutic doses (e.g., 2.5-10 mg/kg).
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| References | |
| Additional Infomation |
Murepavadin TFA is a research-grade antibiotic that has advanced to clinical development for the treatment of hospital-acquired and ventilator-associated pneumonia (HAP/VAP) caused by Pseudomonas aeruginosa. It has not received FDA approval as of current knowledge but represents a promising first-in-class OMPTA. It is not approved for human use as a research compound and is strictly for laboratory research.
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| Molecular Formula |
C73H112N22O16.C2HF3O2
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| Molecular Weight |
1667.83
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| Related CAS # |
Murepavadin;944252-63-5
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~50 mg/mL (~29.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (14.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5996 mL | 2.9979 mL | 5.9958 mL | |
| 5 mM | 0.1199 mL | 0.5996 mL | 1.1992 mL | |
| 10 mM | 0.0600 mL | 0.2998 mL | 0.5996 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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